Table 3.

DMPK Profiling of Early Analogues

no.	cLogPa	LLEb	mGlu3 IC50 (nM)	fold vs mGlu5	rat plasma Fuc		CLplasma (mL/min/kg)d	VSS (L/kg)d
24	3.96	2.38	462	0.20	0.060	95	40	3.5
38	4.24	1.70	1160	>25	0.005	32	82	2.2
47	3.06	3.21	539	>18	0.135	88	82	6.6
48	3.57	2.65	605	4.8	0.034	141	29	5.2

^aCalculated using Dotmatics Elemental (www.dotmatics.com/products/elemental/).

^bLLE (ligand-lipophilicity efficiency) = pIC₅₀ – cLogP.

^cF_u = fraction unbound.

^dRat IV PK results (n = 2); dose = 0.2 mg/kg; solution in 9% EtOH, 37% PEG 400, 54% DMSO (2 mg/mL).